opicapone (Rx)

Brand and Other Names:Ongentys
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule

  • 25mg
  • 50mg

Parkinson Disease

Indicated as an adjunct to levodopa/carbidopa to reduce OFF episodes in patients with Parkinson disease

50 mg PO qHS

Dosage Modifications

Renal impairment

  • Mild-to-moderate (CrCl 30-89 mL/min): No dosage adjustment necessary
  • Severe (CrCl<30 mL/min): Not studied; owing to the potential for increased exposure, monitor for adverse reactions and discontinue therapy if tolerability issues arise
  • End-stage renal disease (ESRD) (CrCl <15 mL/min): Avoid use

Hepatic impairment

  • Mild (Child-Pugh A): No dosage adjustment necessary
  • Moderate (Child-Pugh B): 25 mg PO qHS
  • Severe (Child-Pugh C): Avoid use

Dosing Considerations

When discontinuing therapy, monitor patients and consider adjustment of other dopaminergic therapies as needed

European Drug Information

Click here to view drug information in Europe

Safety and efficacy not established

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Interactions

Interaction Checker

and opicapone

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      Serious - Use Alternative

        Significant - Monitor Closely

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            Adverse Effects

            >10%

            Dyskinesia (20%)

            1-10%

            Constipation (6%)

            Increased blood creatine kinase (5%)

            Hypotension/syncope (5%)

            Hypotension/syncope (5%)

            Decreased weight (4%)

            Hypertension (3%)

            Dry mouth (3%)

            Dizziness (3%)

            Hallucination (3%)

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            Warnings

            Contraindications

            Concomitant use of nonselective monoamine oxidase (MAO) inhibitors

            History of pheochromocytoma, paraganglioma, or other catecholamine-secreting neoplasm

            Cautions

            Patients treated with dopaminergic medications and/or medications that increase levodopa exposure have reported falling asleep while engaged in activities of daily living (eg, operating motor vehicles); advise not to drive and to avoid other potentially dangerous activities

            Hypotension (orthostatic and nonorthostatic), syncope, and presyncope occurred; monitor for hypotension; if hypotension occurs, consider discontinuing or adjusting dosage of other medications that may lower blood pressure

            May potentiate the effects of levodopa and may cause or exacerbate dyskinesia; consider levodopa or dopaminergic medication dose reduction

            Hallucinations, delusions, agitation, or aggressive behavior occurred; consider discontinuing if hallucinations or psychoticlike behaviors occur; avoid treating patients with a major psychotic disorder because of the risk of exacerbating the psychosis with an increase in central dopaminergic tone

            May intensify urges (eg, gambling, increased sexual activity, spending, binge eating) and the inability to control these urges while taking one or more dopaminergic therapies that increase central dopaminergic tone; reevaluate and consider discontinuing therapy if urges develop during treatment

            Symptoms resembling neuroleptic malignant syndrome (characterized by elevated temperature, muscular rigidity, altered consciousness, and autonomic instability), with no other obvious etiology, have been reported in association with rapid dose reduction, withdrawal of, or changes in drugs that increase central dopaminergic tone; when discontinuing therapy, monitor and consider adjustment of other dopaminergic therapies as needed

            Drug interaction overview

            • Opicapone is a substrate of P-gp, BCRP, MRP2, OATP1B2, and OATP2B1 transporters; no clinically significant transporter-mediated interaction is expected for opicapone
            • Nonselective MAO inhibitors
              • Coadministration is contraindicated
              • Concomitant use with nonselective MAO inhibitors (eg, phenelzine, isocarboxazid, tranylcypromine) may inhibit catecholamine metabolism, leading to increased levels of catecholamines
              • Selective MAO-B inhibitors can be used concomitantly with opicapone
            • Drugs metabolized by catechol-O-methyltransferase (COMT)
              • Use with caution
              • Coadministration with drugs metabolized by COMT may affect the pharmacokinetics of those drugs, which may increase the risk of possible arrhythmias, increased heart rate, and excessive changes in blood pressure
              • Monitor for changes in heart rate, rhythm, and blood pressure in patients concomitantly treated with opicapone and drugs metabolized by COMT

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            Pregnancy & Lactation

            Pregnancy

            No adequate data available on use in pregnant females

            Animal data

            • Oral administration during pregnancy resulted in adverse effects on embryofetal development (increased incidence of fetal abnormalities) at clinically relevant plasma exposure in one of two species tested
            • In addition, opicapone is always coadministered with levodopa/carbidopa, which is known to cause development toxicity in rabbits

            Lactation

            No data available on drug presence in human milk and its effects on breastfeeding or milk production

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

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            Pharmacology

            Mechanism of Action

            Once daily, peripheral-acting, COMT inhibitor; decreases conversion rate of levodopa to 3-O-methyldopa, thereby prolonging levodopa half-life to reduce motor fluctuations

            Absorption

            Peak plasma time: 2 hr

            Effects of food

            • After a moderate-fat/moderate-calorie meal, mean peak plasma concentration decreased 62%, mean AUC decreased 31%, delayed peak plasma time by 4 hr

            Distribution

            Protein bound: >99% (independent of concentration)

            Metabolism

            Primary metabolic pathway: Sulphation

            Other metabolic pathways: Glucuronidation, methylation (by COMT), reduction, and glutathione conjugation

            Elimination

            Mean half-life: 1-2 hr

            Excretion

            • Feces: 70% (22% unchanged)
            • Expired: 20%
            • Urine: 5% (<1 unchanged)
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            Administration

            Oral Administration

            Administer at bedtime

            Do not eat food for 1 hr before and for at least 1 hr after administration

            Missed dose: Take dose at the next scheduled time

            Storage

            Capsules: Store at <30ºC (86ºF)

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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
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            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
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            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.